Actinobacteria are Gram-positive bacteria that have a complex multicellular life cycle and are well known for their ability to produce a wide range of bioactive natural products (NPs).

Kinase inhibitors are key therapeutic agents, particularly in oncology, yet their clinical efficacy is often hampered by off-target effects and limited understanding of their cellular target profiles.

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Biological cells, the basic building blocks of all life forms, are surrounded by a lipid membrane. More than half of the membrane is occupied by membrane proteins, which can regulate the cell functionality through specific arrangements.

Following its foundation in 1575, Leiden University was quick to incorporate Roman goddess Minerva in its coat of arms. This explains why Rembrandt’s Minerva from 1635 can be seen on the façade of the Academy Building, which has been in use by the University since 1581. This is where, in the Senate…

As a university, we offer you the best education you can get. Professors, tutors and lecturers are ready to teach and guide you. But we do more than that. Of course, studying is your own responsibility, but we are happy to help if you need support. You decide what and when; online or on campus. These…

The investigations described in this thesis lay out strategies aimed at advancing antibiotic research and development. The examples presented revolve around two main approaches: understanding drug-target interactions and target identification.

Promotores: Prof.dr. H. S. Overkleeft, Prof.dr. G. A. van der Marel

During the early modern period, many medieval manuscripts were cut up into strips of parchment which were reused to reinforce the bindings of newly printed books. Until recently, these reused pieces of medieval manuscripts only came to light when the early modern book binding was damaged and/or subjected…

The institute is funded by the Ministries of Education, Culture and Science and of Foreign Affairs and by Leiden University. To safeguard the institute’s independence and interests in Morocco, it is part of the Netherlands Embassy in Rabat under Moroccan law. The institute performs its tasks under the…

To get a feeling of how we operate at LED3 when it comes to Early Drug Discovery, please browse through our case studies. When you select a case study you’ll find relevant contacts.

This thesis explored the molecular pharmacological mechanisms of targeting CB2R via investigation of novel drug discovery concepts such as target binding kinetics, allosteric modulation and biased signaling.

The main subject of this thesis is the design and synthesis of paramagnetic molecules for protein studies with NMR and EPR spectroscopy.

Structure-affinity relationship (SAR) and structure-kinetics relationship (SKR) studies were combined to investigate a series of biphenyl anthranilic acid agonists for the HCA2 receptor.

Source: Bioorg Med Chem, Volume 23, Issue 14, pp. 4034-49 (2015)

The discovery of new medicines is a tedious and lengthy process. On average, over 10,000 molecules need to be studied for one to become a drug and reach the patient. Part of that process are the very costly clinical trials in humans, and candidate drugs often fail due to side effects or lack of efficacy.…

How can we develop new chemical biology tools and approaches to understand and interfere with glucosylceramide metabolism in relation to Gaucher disease?

Promotor: A.P. IJzerman

Promotor: A.P. IJzerman

Carbohydrates are present on the surface of bacteria making them suitable antigen candidates for vaccine development. This thesis deals with the synthesis of two carbohydrate-based components; the capsular polisaccharide of S. aureus type 5 and teichoic acids from staphilococci and enterococci speci…

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Source: J Med Chem, Volume 57, Issue 8, pp. 3213-22 (2014)

Allosteric modulation has long been recognized as a general and widespread mechanism for the control of protein function. Modulators bind to regulatory sites distinct from the active site on the protein, resulting in conformational changes that may profoundly influence protein function. This concept…

Source: Mediators Inflamm (2014)

Supervisor: Maarten Doornbos

Supervisor: Lizi Xia